Particulate composition comprising bioactive substance and method of producing the same

Abstract

The present invention provides a particulate composition wherein an oil component (A) comprising a water-insoluble bioactive substance is poly-dispersed while forming a domain in a matrix comprising of a water-soluble excipient based on a water-soluble polymer, and wherein the sphericity of the particulate composition is not less than 0.9 and a method of producing the same. The particulate composition simultaneously has excellent water solubility, workability, tabletability and heat-resistance. It also provides a food, food with nutrient function claims, food for specified health uses, nutritional supplement, nutritional product, animal drug, drink, feed, pet food, cosmetic, pharmaceutical product, therapeutic drug, prophylactic drug and the like, which contain the particulate composition.

1 . A particulate composition wherein an oil component (A) comprising a water-insoluble bioactive substance is poly-dispersed while forming a domain in a matrix comprising a water-soluble excipient based on a water-soluble polymer, and wherein the sphericity is not less than 0.9.  
     
     
         2 . The particulate composition of  claim 1 , wherein the water-insoluble bioactive substance is at least one kind selected from the group consisting of oxidized coenzyme Q10, an unsaturated fatty acid, an oil-soluble vitamin, a plant hydrophobic extract ingredient and a carotenoid.  
     
     
         3 . The particulate composition of  claim 1 , wherein the oil component (A) is poly-dispersed while forming not less than five domains.  
     
     
         4 . The particulate composition of  claim 1 , wherein the water-soluble polymer is at least one kind selected from the group consisting of gum arabic, ghatti gum, agar, starch, pectin, carrageenan, casein, dried albumen, curdlan, alginic acids, soybean polysaccharide, pullulan, celluloses, xanthan gum, carmellose salt and polyvinylpyrrolidone.  
     
     
         5 . The particulate composition of  claim 2 , wherein the unsaturated fatty acid is at least one kind selected from the group consisting of oleic acid, linoleic acid, conjugated linoleic acid, linolenic acid, arachidonic acid, docosahexaenoic acid, docosapentaenoic acid and eicosapentaenoic acid.  
     
     
         6 . The particulate composition of  claim 2 , wherein the oil-soluble vitamin is at least one kind selected from the group consisting of vitamin A, vitamin D, vitamin E, vitamin K, and derivatives thereof.  
     
     
         7 . The particulate composition of  claim 2 , wherein the plant hydrophobic extract ingredient is obtained from at least one kind of plants or plant-processed products selected from the group consisting of licorice, turmeric,  perilla , clove, cinnamon, ginger, lemongrass, peppermint, dokudami ( Houttuyania cordata ),  coix  seed, rice bran, cornflower, fennel, boxthorn,  zanthoxylum, nasturtium, dioscorea , sanryo, kinkaran ( Tinospora capillipes ), amachazuru ( Gynostema pentaphyllum ), thuja, hakutouou ( Pulsatilla chinensis ), parsley, onion, nutmeg, wild-rice, gluten feed, tobiko (konnyaku byproduct powder), paprika, horseradish, lemon,  capsicum , sesame, spearmint and leaf mustard.  
     
     
         8 . The particulate composition of  claim 1 , wherein the oil component (A) comprises 1 to 100 wt % of a bioactive substance, 0 to 99 wt % of a fat and oil, and 0 to 99 wt % of a surfactant (D).  
     
     
         9 . The particulate composition of  claim 8 , wherein the surfactant (D) is at least one kind selected from the group consisting of glycerol fatty acid ester, polyglycerin ester, sucrose fatty acid ester, sorbitan fatty acid ester, and propylene glycol fatty acid ester, each having an HLB of not more than 10, and lecithins.  
     
     
         10 . The particulate composition of  claim 1 , wherein the content of the bioactive substance in the particulate composition is 1-70 wt %.  
     
     
         11 . The particulate composition of  claim 1 , wherein the volume average particle size is 1-1000 μm.  
     
     
         12 . The particulate composition of  claim 1 , wherein the average particle size of the domain(s) is 0.01 to 50 μm.  
     
     
         13 . The particulate composition of  claim 1 , wherein a light-fast ingredient is contained in the composition.  
     
     
         14 . The particulate composition of  claim 13 , wherein the light-fast ingredient is at least one kind selected from the group consisting of titanium oxide, food colors, red iron oxide pigment, safflower pigment, annatto pigment, caramel pigment, gardenia pigment, tar pigment and chlorophyll.  
     
     
         15 . An emulsified aqueous solution prepared by dissolving the particulate composition of  claim 1  in water, wherein a median diameter of the emulsified particles in emulsified aqueous solution is not more than 2 μm.  
     
     
         16 . A method of producing a particulate composition comprising a bioactive substance, comprising suspending an oil-in-water emulsified composition prepared from an oil component (A) comprising a water-insoluble bioactive substance and an aqueous solution comprising a water-soluble excipient based on a water-soluble polymer in an oil component (B), and thereafter removing the water in the emulsified composition in the oil component (B).  
     
     
         17 . The method of  claim 16 , wherein the oil component (B) comprises 0-99.99 wt % of fat and oil and 0.01-100 wt % of surfactant (E).  
     
     
         18 . The method of  claim 16 , wherein the surfactant (E) is at least one kind selected from the group consisting of glycerol fatty acid ester, polyglycerin ester, sucrose fatty acid ester and sorbitan fatty acid ester, each having an HLB of not more than 10, and lecithins.  
     
     
         19 . The method of  claim 16 , wherein the obtained particulate composition has a sphericity of not less than 0.9.  
     
     
         20 . The method of  claim 16 , wherein the water-soluble polymer is at least one kind selected from the group consisting of gum arabic, ghatti gum, agar, starch, pectin, carrageenan, casein, dried albumen, curdlan, alginic acids, soybean polysaccharide, pullulan, celluloses, xanthan gum, carmellose salt and polyvinylpyrrolidone.  
     
     
         21 . The method of production of  claim 16 , wherein the oil component (A) comprises 1 to 100 wt % of a bioactive substance, 0 to 99 wt % of a fat and oil, and 0 to 99 wt % of a surfactant (D).  
     
     
         22 . The method of production of  claim 16 , wherein the water-insoluble bioactive substance is at least one kind selected from the group consisting of oxidized coenzyme Q10, an unsaturated fatty acid, an oil-soluble vitamin, a plant hydrophobic extract ingredient and a carotenoid.  
     
     
         23 . The method of  claim 21 , wherein the surfactant (D) is at least one kind selected from the group consisting of glycerol fatty acid ester, polyglycerin ester, sucrose fatty acid ester, sorbitan fatty acid ester and propylene glycol fatty acid ester, each having an HLB of not more than 10, and lecithins.